1202757-89-8 Manufacturer Hot Sale 1202757-89-8 AVL 292 High Purity Spebrutinib

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1202757-89-8 Manufacturer Hot Sale 1202757-89-8 AVL 292 High Purity Spebrutinib

Spebrutinib, also known as AVL-292 or CC-292, is an orally bioavailable, selective inhibitor of BrutonÂ’s agammaglobulinemia tyrosine kinase (BTK), with potential antineoplastic activity. Upon administration, AVL-292 targets and covalently binds to BTK, thereby preventing its activity. By irreversibly inhibiting BTK, administration of this agent may lead to an inhibition of B cell receptor (BCR) signaling and may inhibit cell proliferation of B-cell malignancies.

Spebrutinib (CC-292) is a covalent, highly selective, orally active inhibitor of Btk with IC₅₀ value of 0.5 nM. Spebrutinib also less potently inhibits Yes, c-Src, Brk, Lyn, and Fyn with IC₅₀s of 723 nM, 1.729 μM, 2.43 μM, 4.4 μM, and 7.15 μM, rspectively. Extensive analysis has revealed that the EC₅₀ of Btk occupancy from a Spebrutinib dose-response in Ramos cells (EC₅₀=6 nM) correlated directly with the cellular EC₅₀ of Btk kinase inhibition with Spebrutinib (EC₅₀=8 nM). Furthermore, the concentration at which Spebrutinib inhibits 90% of Btk activity in Ramos cells is 35 nM while the concentration of Spebrutinib required for 90% occupancy of Btk is 39 nM

AVL-292 is a covalent inhibitor of Bruton’s tyrosine kinase (BTK; IC₅₀ = 5.9 nM). It is selective for BTK over a panel of 61 kinases when used at a concentration of 1 µM but does inhibit the additional Tec family kinases BMX, Itk, Tec, and TXK (IC₅₀s = 0.7, 36, 6.2, and 8.9 nM, respectively). AVL-292 inhibits naïve human B cell proliferation (EC₅₀ = 3 nM). It reduces joint damage, pannus formation, cartilage degradation, and bone erosion in a mouse model of rheumatioid arthritis induced by collagen when used at doses of 3, 10, and 30 mg/kg.